Assay of Secoverine and Active Metabolites: Comparison of Stable Isotope Dilution with Receptor Binding Assay

  • H. de Bree
  • P. H. van Amsterdam
  • D. J. K. van der Stel
  • M. Th. M. Tulp
  • W. R. Vincent
  • L. W. de Zoeten
Part of the Methodological Surveys in Biochemistry and Analysis book series (MSBA, volume 14)

Abstract

Secoverine (formula below) is a new gastro-intestinal muscle relaxant whose pharmacokinetics and disposition are currently being investigated in different animal species and man. The drug is administered as a racemate of which only the (+) enantiomer has pharmacological activity. Human pharmacology revealed activity after either oral or parenteral administration. Plasma levels of the parent drug were hardly measurable (<1 ng/ml) after oral administration, whereas a similar i.v. dose resulted in plasma levels of ~10 ng/ml. Accordingly we investigated the occurrence of active metabolites. As urinary metabolite profiles did not provide any clue in this respect, we started in vitro experiments with 14C-labelled secoverine.

Keywords

Heptane Seco Trimethyl Rine Mandel 

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Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • H. de Bree
    • 1
  • P. H. van Amsterdam
    • 1
  • D. J. K. van der Stel
    • 1
  • M. Th. M. Tulp
    • 1
  • W. R. Vincent
    • 1
  • L. W. de Zoeten
    • 1
  1. 1.Duphar Research LaboratoriesWeespThe Netherlands

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